Optimization of M(4) positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

This letter describes the further chemical optimization of the 5-amino-thieno[2,3-c]pyridazine series (VU0467154/VU0467485) of M(4) positive allosteric modulators (PAMs), developed via iterative parallel synthesis, culminating in the discovery of the non-human primate (NHP) in vivo tool compound, VU...

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Publicat a:Bioorg Med Chem Lett
Autors principals: Melancon, Bruce J., Wood, Michael R., Noetzel, Meredith J., Nance, Kellie D., Engelberg, Eileen M., Han, Changho, Lamsal, Atin, Chang, Sichen, Cho, Hyekyung P., Byers, Frank W., Bubser, Michael, Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Engers, Darren W., Wu, Dedong, Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Format: Artigo
Idioma:Inglês
Publicat: 2017
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Article
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5508548/
https://ncbi.nlm.nih.gov/pubmed/28442253
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.04.043
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